CN103003231A - 制备苯基环丙基胺衍生物的新方法及其用于制备替卡格雷的用途 - Google Patents

制备苯基环丙基胺衍生物的新方法及其用于制备替卡格雷的用途 Download PDF

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CN103003231A
CN103003231A CN2011800322620A CN201180032262A CN103003231A CN 103003231 A CN103003231 A CN 103003231A CN 2011800322620 A CN2011800322620 A CN 2011800322620A CN 201180032262 A CN201180032262 A CN 201180032262A CN 103003231 A CN103003231 A CN 103003231A
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formula
acid
solvent
heterogeneous forms
stereochemistry heterogeneous
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A·S·希勒
V·奈尔
N·特里维迪
N·S·普拉汉
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Actavis Group PTC ehf
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/62—Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/54—Preparation of compounds containing amino groups bound to a carbon skeleton by rearrangement reactions
    • C07C209/56—Preparation of compounds containing amino groups bound to a carbon skeleton by rearrangement reactions from carboxylic acids involving a Hofmann, Curtius, Schmidt, or Lossen-type rearrangement
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/35—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/39—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton
    • C07C211/40—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of an unsaturated carbon skeleton containing only non-condensed rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/16—Systems containing only non-condensed rings with a six-membered ring the ring being unsaturated

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2011800322620A 2010-06-30 2011-06-28 制备苯基环丙基胺衍生物的新方法及其用于制备替卡格雷的用途 Pending CN103003231A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
IN1841CH2010 2010-06-30
IN1841/CHE/2010 2010-06-30
IN2043CH2010 2010-07-19
IN2043/CHE/2010 2010-07-19
PCT/IB2011/002246 WO2012001531A2 (fr) 2010-06-30 2011-06-28 Nouveaux procédés pour la préparation de dérivés de phénylcyclopropylamine et leur utilisation pour la préparation de ticagrelor

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CN103003231A true CN103003231A (zh) 2013-03-27

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CN2011800322620A Pending CN103003231A (zh) 2010-06-30 2011-06-28 制备苯基环丙基胺衍生物的新方法及其用于制备替卡格雷的用途

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US (2) US20130165696A1 (fr)
EP (1) EP2588441A2 (fr)
JP (1) JP2013530209A (fr)
CN (1) CN103003231A (fr)
AU (1) AU2011273101A1 (fr)
BR (1) BR112012033500A2 (fr)
CA (1) CA2803354A1 (fr)
MX (1) MX2012014793A (fr)
RU (1) RU2013103794A (fr)
WO (1) WO2012001531A2 (fr)
ZA (1) ZA201300002B (fr)

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106905182A (zh) * 2017-01-12 2017-06-30 淮阴工学院 一种替格瑞洛中间体的合成方法及其中间体
CN107141236A (zh) * 2017-04-24 2017-09-08 台州职业技术学院 替卡格雷中间体(1r,2r)‑2‑(3,4‑二氟代苯基)环丙烷腈的新合成方法
CN108129251A (zh) * 2017-12-22 2018-06-08 上海应用技术大学 一种2-乙基苯乙烯的合成工艺
CN111763209A (zh) * 2015-12-31 2020-10-13 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺

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TWI229674B (en) 1998-12-04 2005-03-21 Astra Pharma Prod Novel triazolo[4,5-d]pyrimidine compounds, pharmaceutical composition containing the same, their process for preparation and uses
WO2010084160A1 (fr) 2009-01-21 2010-07-29 Oryzon Genomics S.A. Dérivés de phénylcyclopropylamine et leur utilisation médicale
RU2602814C2 (ru) 2009-09-25 2016-11-20 Оризон Дженомикс С.А. Лизинспецифические ингибиторы деметилазы-1 и их применение
US8946296B2 (en) 2009-10-09 2015-02-03 Oryzon Genomics S.A. Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
US9616058B2 (en) 2010-02-24 2017-04-11 Oryzon Genomics, S.A. Potent selective LSD1 inhibitors and dual LSD1/MAO-B inhibitors for antiviral use
WO2011106573A2 (fr) 2010-02-24 2011-09-01 Oryzon Genomics, S.A. Inhibiteurs de la lysine déméthylase utilisés dans le traitement et la prévention de maladies et de troubles associés à hepadnaviridae
HUE030938T2 (en) 2010-04-19 2017-06-28 Oryzon Genomics Sa Lysine-specific demethylase-1 inhibitors and their use
WO2012013727A1 (fr) 2010-07-29 2012-02-02 Oryzon Genomics S.A. Dérivés de cyclopropylamine utiles en tant qu'inhibiteurs de lsd1
CN103124724B (zh) 2010-07-29 2015-05-20 奥瑞泽恩基因组学股份有限公司 Lsd1的基于芳基环丙胺的脱甲基酶抑制剂及其医疗用途
WO2012045883A1 (fr) 2010-10-08 2012-04-12 Oryzon Genomics S.A. Inhibiteurs d'oxydases de cyclopropylamine
WO2012072713A2 (fr) 2010-11-30 2012-06-07 Oryzon Genomics, S.A. Inhibiteurs de la déméthylase spécifique de la lysine pour des maladies et troubles liés aux flaviviridés
RU2013133879A (ru) * 2010-12-20 2015-01-27 Актавис Груп Птс Ехф НОВЫЕ СПОСОБЫ ПОЛУЧЕНИЯ ТРИАЗОЛО[4, 5-d]ПИРИМИДИНА, ЕГО ПРОИЗВОДНЫЕ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ
EP2712315B1 (fr) 2011-02-08 2021-11-24 Oryzon Genomics, S.A. Inhibiteurs de lysine déméthylase pour des troubles myéloprolifératifs
RU2681211C2 (ru) 2011-10-20 2019-03-05 Оризон Дженомикс С.А. (гетеро)арилциклопропиламины в качестве ингибиторов lsd1
BR112014009238B1 (pt) 2011-10-20 2022-08-09 Oryzon Genomics S.A. Compostos de (hetero)aril ciclopropilamina, seus usos e composições farmacêuticas
EP2628721A1 (fr) 2012-02-20 2013-08-21 LEK Pharmaceuticals d.d. Synthèse de l'acide 2-(3,4-difluorophényl) cyclopropanecarboxylique
EP2644590A1 (fr) 2012-03-30 2013-10-02 LEK Pharmaceuticals d.d. Synthèse de dérivés et sels de 2-(3,4-difluorophényl) cyclopropanamine
CN104603098B (zh) 2012-03-30 2016-06-29 桑多斯股份公司 2-(3,4-二氟苯基)环丙胺衍生物和盐的合成
WO2013150495A2 (fr) 2012-04-05 2013-10-10 Dr. Reddy's Laboratories Limited Préparation de ticagrelor
WO2013163892A1 (fr) * 2012-05-02 2013-11-07 Sunshine Lake Pharma Co., Ltd. Nouveaux composés de triazolopyrimidine et leur procédé de préparation
JP2015534464A (ja) 2012-10-09 2015-12-03 カリフォルニア インスティチュート オブ テクノロジー ヘム酵素によって触媒されるインビボおよびインビトロオレフィンシクロプロパン化
CN103073525B (zh) * 2013-02-04 2015-01-28 北京科技大学 一种合成制备(s)-(3,4-二氟苯基)环氧己烷的方法
WO2014206187A1 (fr) 2013-06-24 2014-12-31 苏州明锐医药科技有限公司 Procédé de préparation du ticagrelor et de ses intermédiaires
WO2015162630A1 (fr) 2014-04-25 2015-10-29 Anlon Chemical Research Organization Nouveaux procédés de préparation de triazolo[4,5-d]-pyrimidines, dont le ticagrelor, via de nouveaux intermédiaires et une nouvelle voie de synthèse
WO2016116942A1 (fr) 2015-01-20 2016-07-28 Anlon Chemical Research Organization Nouveaux composés pharmaceutiques comprenant du ticagrélor avec des sels d'aspirine
WO2016117852A2 (fr) * 2015-01-22 2016-07-28 동아에스티 주식회사 Procédé pour la préparation du ticagrelor et nouveaux intermédiaires à cet effet
EP3303267A4 (fr) * 2015-05-26 2019-04-24 California Institute of Technology Catalyseurs à base d'hémoprotéines permettant d'améliorer la synthèse énantiosélective enzymatique du ticagrelor
CN106854158B (zh) * 2016-12-08 2019-06-14 淮阴工学院 一种替格瑞洛中间体的合成方法及其中间体

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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111763209A (zh) * 2015-12-31 2020-10-13 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
CN111763209B (zh) * 2015-12-31 2021-12-03 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
CN106905182A (zh) * 2017-01-12 2017-06-30 淮阴工学院 一种替格瑞洛中间体的合成方法及其中间体
CN107141236A (zh) * 2017-04-24 2017-09-08 台州职业技术学院 替卡格雷中间体(1r,2r)‑2‑(3,4‑二氟代苯基)环丙烷腈的新合成方法
CN107141236B (zh) * 2017-04-24 2019-03-22 台州职业技术学院 替卡格雷中间体(1r,2r)-2-(3,4-二氟代苯基)环丙烷腈的新合成方法
CN108129251A (zh) * 2017-12-22 2018-06-08 上海应用技术大学 一种2-乙基苯乙烯的合成工艺

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Publication number Publication date
BR112012033500A2 (pt) 2016-11-29
MX2012014793A (es) 2013-03-05
RU2013103794A (ru) 2014-08-10
AU2011273101A1 (en) 2013-01-17
US20140350301A1 (en) 2014-11-27
EP2588441A2 (fr) 2013-05-08
JP2013530209A (ja) 2013-07-25
ZA201300002B (en) 2014-05-28
US20130165696A1 (en) 2013-06-27
WO2012001531A3 (fr) 2012-08-16
WO2012001531A2 (fr) 2012-01-05
CA2803354A1 (fr) 2012-01-05

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Application publication date: 20130327